Suberoyl bis-hydroxamic acid (Synonyms:Suberohydroxamic acid; SBHA)
目录号 : KM18134 CAS No. : 38937-66-5 纯度 : ≥98%

Suberoyl bis-hydroxamic acid (Suberohydroxamic acid; SBHA) 是竞争性且可透过细胞的 HDAC1 和 HDAC3 抑制剂,ID50 值分别为 0.25 μM 和 0.30 μM。Suberoyl bis-hydroxamic acid 使肿瘤细胞易于凋亡 (apoptosis) 并促进线粒体凋亡途径。Suberoyl bis-hydroxamic acid 可用于甲状腺髓样癌 (MTC) 的研究。

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生物活性

Suberoyl bis-hydroxamic acid (Suberohydroxamic acid; SBHA) is a competitive and cell-permeable HDAC1 and HDAC3 inhibitor with ID50 values of 0.25 μM and 0.30 μM, respectively.Suberoyl bis-hydroxamic acid renders MM cells susceptible to apoptosis and facilitates the mitochondrial apoptotic pathways.Suberoyl bis-hydroxamic acid can be used for the study of medullary thyroid carcinoma (MTC).

体外研究

Suberoyl bis-hydroxamic acid (10, 20 or 50 μM; 24 hours) combination with TRAIL improves apoptosis extent, and when TRAIL is combined with 20 μM SBHA (itself causing only 10–15% apoptosis), resulting in 45–50% cell death.
Suberoyl bis-hydroxamic acid (20-50 μM; 10-20 hours) alone has little effect on the expression of the proteins Bcl-xL, Mcl-1, and has albeit mildeffect on Bax. When it combines with TRAIL,which increases the ratio of relative protein expression of Bcl-xL and Bax in early periods, while the change in the ratio of Mcl-1 and Bax increases later in MM-BI and Ist-Mes2 cells.
Suberoyl bis-hydroxamic acid (30 μM; 6 hours) causes accumulation of acetylated histone H4 in MEL cells.

Apoptosis Analysis

Cell Line: MM-BI and Ist-Mes2 cells
Concentration: 10 μM, 20 μM or 50 μM
Incubation Time: 24 hours
Result: Showed a cooperative effect in cell apoptosis.
体内研究

Suberoyl bis-hydroxamic acid (intraperitoneal injection; 200 mg/kg; every 2 days; 12 days) reveals a marked increase in the active form of Notch1 (NICD) with a concomitant decrease in ASCL1. It reduces the MTC tumor growth.

Animal Model: Nude mice injected with human MTC cells
Dosage: 200 mg/kg
Administration: Intraperitoneal injection; every 2 days; 12 days
Result: Resulted in an average 55% inhibition of tumor growth in SBHA treatment group.
分子式
C8H16N2O4
分子量
204.22
CAS号
38937-66-5
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (244.83 mM; Need ultrasonic)

H2O : 8.33 mg/mL (40.79 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.8967 mL 24.4834 mL 48.9668 mL
5 mM 0.9793 mL 4.8967 mL 9.7934 mL
10 mM 0.4897 mL 2.4483 mL 4.8967 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (12.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (12.24 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (12.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (12.24 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (12.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (12.24 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
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This equation is commonly abbreviated as: C1V1 = C2V2
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